AZD-5438

SKU: orb1305380

Description

AZD-5438

Research Area

Cell Biology

Key Properties

• CAS Number: 602306-29-6
• MW: 371.46
• Purity: 99.23%
• Formula: C₁₈H₂₁N₅O₂S
• SMILES: CC(C)n1c(C)ncc1-c1ccnc(Nc2ccc(cc2)S(C)(=O)=O)n1
• Target: CDK
• Solubility: Ethanol:63 mg/mL (169.6 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.38 mM);DMSO:74 mg/mL (199.21 mM)

Bioactivity

• Target IC50:
  CDK5-p25:14 nM|CDK1:16 nM|CDK7-CyclinH:821 nM|CDK4-CyclinD1:449 nM|CDK2-CyclinA:45 nM|CDK2:6 nM|CDK6-CyclinD1:21 nM|CDK9:20 nM
• In Vivo:
  AZD5438 effectively inhibits the kinase activity of p25-cdk5 and glycogen synthase kinase 3β, with IC50 values of 14 nM and 17 nM, respectively. In various tumor cell lines (lung, colorectal, breast, prostate, and blood tumors), AZD5438 (IC50=0.2-1.7 μM) induces cell cycle arrest and inhibits cell proliferation by hindering the phosphorylation of cdk-dependent substrates. Furthermore, AZD5438 demonstrates potent inhibition of cyclin-dependent kinases (cdks) including E-cdk2 (IC50=6 nM), A-cdk2 (IC50=45 nM), B1-cdk1 (IC50=16 nM), D3-cdk6 (IC50=21 nM), and T-cdk9 (IC50=20 nM), showcasing its broad efficacy in targeting various components of the cell cycle mechanism.
• In Vitro:
  In the SW620 xenograft model, AZD5438 exhibits dose-dependent inhibition on various cell cycle proteins, such as phospho-histone H3 (phH3), phospho-nucleophosmin, and PP1a. AZD5438, administered orally, demonstrates tumor-suppressive effects across various cancer types including breast, colon, lung, prostate, and ovarian cancers.
• Cell Research:
  AZD5438 is tested against solid tumor cell lines. Briefly, cells are incubated for 48 hours with AZD5438 at a range of concentrations. At the end of incubation, the cells are pulsed with 5-bromo-2′-deoxyuridine (BrdUrd) and the amount of DNA synthesis is measured. The IC50 for inhibition of proliferation is specifically determined independently of cell death. Multiple myeloma cell lines are seeded into 96-well plates in RPMI 1640 supplemented with 10% FCS and glutamine and dosed with AZD5438 for 72 hours. Cell growth is measured using AlamarBlue and GI50 values are calculated with reference to pretreatment control values.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cyclin dependent kinase, CDK9, CDK1, CDK, CDK2, AZD 5438, AZD5438, AZD-5438, Inhibitor, inhibit

Compound Identifiers

PubChem CID

16747683